APG-1387

Research use only, not for human use.

APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).

APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells.Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. Western Blot AnalysisCell Line:HepG2 and HCCLM3 cellsConcentration:0.02, 0.2, 2, 20 μM Incubation Time:1, 6, 24 hours Result:Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner.Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.

Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice.Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice. Animal Model:Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells Dosage:20 mg/kg Administration:I.p. every 3 days for 4 weeks Result:Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression.Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.

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Apoptosis

IAP

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1570231-89-8

1157.4

C??H??N??O??S?

>98% (HPLC)

DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)

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(-20℃)

With Ice Pack

≥ 2 years